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Page 1
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
Barrow JC, Stauffer SR, Rittle KE, Ngo PL, Yang Z, Selnick HG, Graham SL, Munshi S, McGaughey GB, Holloway MK, Simon AJ, Price EA, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Espeseth AS, Xu M, Huang Q, Wolfe A, Pietrak B, Zuck P, Levorse DA, Hazuda D, Vacca JP. Barrow JC, et al. Among authors: colussi d. J Med Chem. 2008 Oct 23;51(20):6259-62. doi: 10.1021/jm800914n. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811140
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.
Barrow JC, Nantermet PG, Stauffer SR, Ngo PL, Steinbeiser MA, Mao SS, Carroll SS, Bailey C, Colussi D, Bosserman M, Burlein C, Cook JJ, Sitko G, Tiller PR, Miller-Stein CM, Rose M, McMasters DR, Vacca JP, Selnick HG. Barrow JC, et al. Among authors: colussi d. J Med Chem. 2003 Dec 4;46(25):5294-7. doi: 10.1021/jm034141y. J Med Chem. 2003. PMID: 14640538
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Rajapakse HA, Nantermet PG, Selnick HG, Munshi S, McGaughey GB, Lindsley SR, Young MB, Lai MT, Espeseth AS, Shi XP, Colussi D, Pietrak B, Crouthamel MC, Tugusheva K, Huang Q, Xu M, Simon AJ, Kuo L, Hazuda DJ, Graham S, Vacca JP. Rajapakse HA, et al. Among authors: colussi d. J Med Chem. 2006 Dec 14;49(25):7270-3. doi: 10.1021/jm061046r. J Med Chem. 2006. PMID: 17149856
Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1.
Barrow JC, Rittle KE, Ngo PL, Selnick HG, Graham SL, Pitzenberger SM, McGaughey GB, Colussi D, Lai MT, Huang Q, Tugusheva K, Espeseth AS, Simon AJ, Munshi SK, Vacca JP. Barrow JC, et al. Among authors: colussi d. ChemMedChem. 2007 Jul;2(7):995-9. doi: 10.1002/cmdc.200700038. ChemMedChem. 2007. PMID: 17458843 No abstract available.
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Lindsley SR, Moore KP, Rajapakse HA, Selnick HG, Young MB, Zhu H, Munshi S, Kuo L, McGaughey GB, Colussi D, Crouthamel MC, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Simon AJ, Seabrook GR, Hazuda DJ, Pudvah NT, Hochman JH, Graham SL, Vacca JP, Nantermet PG. Lindsley SR, et al. Among authors: colussi d. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4057-61. doi: 10.1016/j.bmcl.2007.04.072. Epub 2007 Apr 27. Bioorg Med Chem Lett. 2007. PMID: 17482814
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.
Stanton MG, Stauffer SR, Gregro AR, Steinbeiser M, Nantermet P, Sankaranarayanan S, Price EA, Wu G, Crouthamel MC, Ellis J, Lai MT, Espeseth AS, Shi XP, Jin L, Colussi D, Pietrak B, Huang Q, Xu M, Simon AJ, Graham SL, Vacca JP, Selnick H. Stanton MG, et al. Among authors: colussi d. J Med Chem. 2007 Jul 26;50(15):3431-3. doi: 10.1021/jm070272d. Epub 2007 Jun 21. J Med Chem. 2007. PMID: 17583334
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Moore KP, Zhu H, Rajapakse HA, McGaughey GB, Colussi D, Price EA, Sankaranarayanan S, Simon AJ, Pudvah NT, Hochman JH, Allison T, Munshi SK, Graham SL, Vacca JP, Nantermet PG. Moore KP, et al. Among authors: colussi d. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5831-5. doi: 10.1016/j.bmcl.2007.08.040. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17827011
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.
Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel MC, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, Hazuda D, Hochman JH, Holloway K, Jin L, Kahana J, Lai MT, Lineberger J, McGaughey G, Moore KP, Nantermet P, Pietrak B, Price EA, Rajapakse H, Stauffer S, Steinbeiser MA, Seabrook G, Selnick HG, Shi XP, Stanton MG, Swestock J, Tugusheva K, Tyler KX, Vacca JP, Wong J, Wu G, Xu M, Cook JJ, Simon AJ. Sankaranarayanan S, et al. Among authors: colussi d. J Pharmacol Exp Ther. 2009 Jan;328(1):131-40. doi: 10.1124/jpet.108.143628. Epub 2008 Oct 14. J Pharmacol Exp Ther. 2009. PMID: 18854490
81 results